| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| L647702-5mg |
5mg |
期货  |
| |
| L647702-10mg |
10mg |
期货 |
|
| 规格或纯度 | ≥99% |
|---|---|
| 英文名称 | LHVS |
| 生化机理 | LHVS 是一种强效、非选择性、不可逆、细胞渗透性半胱氨酸蛋白酶和酪蛋白酶抑制剂。LHVS 可减少肌动蛋白环的形成。LHVS 可抑制淋球菌入侵，其 IC 50 为 10 μM。 |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
LHVS is a potent, non-selective, irreversible, cell-permeable cysteine protease and cathepsin inhibitor. LHVS decreases actin ring formation. LHVS inhibits T. gondii invasion with an IC 50 of 10 μM In Vitro LHVS (5 μM, 2 h) results in a 50% reduction of actin ring formation in wild-type osteoclasts when compared with untreated osteoclasts. LHVS acts in a dose-dependent manner on osteoclasts and at 5 μM, LHVS inhibits cathepsins K, L, S, and B. LHVS (1-5 nM) can inhibit specifically cathepsin S in HOM2 cells, leaving other cysteine proteases functionally active. LHVS impairs tachyzoite attachment by blocking the release of at least two key invasion proteins, MIC2 and M2AP, from the micronemes. LHVS (50 μM) selectively impairs microneme protein secretion. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo LHVS (3-30 mg/kg, SC, once) shows anti-hyperalgesic effect in neuropathic rats. LHVS (30 nmol per rat, spinal delivery, daily) is antinociceptive in neuropathic rats. LHVS (1-50 nmol per rat, Intrathecal injection, daily) reverses established neuropathic mechanical hyperalgesia in 14-day neuropathic rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Wistar rats (180-220 g)Dosage: 3-30 mg/kg Administration: SC, once Result: Produced a dose-dependent reversal of the mechanical hyperalgesia which lasted up to 3 h in neuropathic rats. In contrast, a single systemic administration of LHVS did not reverse mechanical allodynia in neuropathic rats. Animal Model: Male Wistar rats received a partial ligation of the left sciatic nerve (PNL)Dosage: 30 nmol per rat Administration: Spinal delivery, Daily Result: Failed to prevent the development of allodynia when continuous delivery from day 0 to day 7 post-PNL, but significantly reversed allodynia on day 7 post-PNL. In addition, the delivery of LHVS from day 7 to day 14 post-PNL significantly reversed established mechanical allodynia from day 8. Animal Model: Male Wistar rats received a partial ligation of the left sciatic nerve (PNL)Dosage: 1, 10 or 50 nmol per rat Administration: Intrathecal injection, Daily Result: Reduced established mechanical hyperalgesia. This effect was dose-dependent and remained significant until 3 h after administration of the highest dose. Form:Solid IC50& Target:cathepsin S cathepsin K cathepsin L Cathepsin B |
| 纯度 | ≥99% |
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 小分子 |
|---|---|
| IIUPAC Name | N-[(2R)-1-[[(E,3R)-1-(benzenesulfonyl)-5-phenylpent-1-en-3-yl]amino]-4-methyl-1-oxopentan-2-yl]morpholine-4-carboxamide |
| INCHI | 1S/C28H37N3O5S/c1-22(2)21-26(30-28(33)31-16-18-36-19-17-31)27(32)29-24(14-13-23-9-5-3-6-10-23)15-20-37(34,35)25-11-7-4-8-12-25/h3-12,15,20,22,24,26H,13-14,16-19,21H2,1-2H3,(H,29,32)(H,30,33)/b20-15+/t24-,26-/m1/s1 |
| InChi Key | YUMYYTORLYHUFW-ZUDLOMHPSA-N |
| Smiles | CC(C)CC(C(=O)NC(CCC1=CC=CC=C1)C=CS(=O)(=O)C2=CC=CC=C2)NC(=O)N3CCOCC3 |
| Isomeric SMILES | CC(C)C[C@H](C(=O)N[C@H](CCC1=CC=CC=C1)/C=C/S(=O)(=O)C2=CC=CC=C2)NC(=O)N3CCOCC3 |
| PubChem CID | 23648296 |
| 分子量 | 527.68 |
| 溶解性 | DMSO : 100 mg/mL (189.51 mM; Need ultrasonic) |
|---|
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